四季青水煎液体外抗内毒素、抗菌和体内抗炎作用

The anti-endotoxin, antibacterial effects in vitro and anti-inflammatory effects in vivo of Ilicis chinensis folium water decoction

目的研究四季青水煎液的抗内毒素、抗菌和抗炎作用,揭示四季青清热解毒作用的药效学特点。方法采用体外鲎试剂凝集实验方法检测其抗内毒素作用;采用琼脂二倍稀释法测定四季青水煎液以及与头孢噻肟、左氧氟沙星和庆大霉素联合使用时对25株甲氧西林敏感金黄色葡萄球菌(MSSA)、耐甲氧西林金黄色葡萄球菌(MRSA)、产超广谱β-内酰胺酶(extended-spectrumβ-lactamase,ESBLs)大肠埃希菌、非产ESBLs大肠埃希菌和铜绿假单胞菌的最低抑菌浓度(minimum inhibitory concentration,MIC);采用二甲苯致小鼠耳廓炎症肿胀法观察其抗炎作用。结果四季青水煎液在生药浓度6.25~100mg/m L时具有抗内毒素作用;对受试菌株MSSA、MRSA的MIC范围均为8~33mg/m L,对产ESBLs大肠埃希菌及非产ESBLs大肠埃希菌的MIC范围均为33~>133mg/m L,对铜绿假单胞菌的MIC为33~133mg/m L;与头孢噻肟、左氧氟沙星和庆大霉素联合使用时抗菌活性有相加作用,分级抑菌浓度(fractional inhibitory concentration,FIC)指数范围为0.5<FIC≤1;在小鼠口服给药剂量1,280~2,000mg/kg时对小鼠耳肿胀具有抗炎作用。结论四季青水煎液具有较强的抗内毒素作用和一定的抗炎作用,对MSSA、MRSA、产ESBLs大肠埃希菌、非产ESBLs大肠埃希菌和铜绿假单胞菌均具有一定的抗菌活性;与头孢噻肟、左氧氟沙星和庆大霉素联合使用时抗菌活性具有相加作用;其清热解毒功能主要以清热作用为主。

Objective To investigate the anti-endotoxin, antibacterial and anti-inflammatory effects of llicis chinensis folium water decoction （ICFWD） and reveal the pharmacological properties of the clearing-heat and detoxifying effects of Ilicis chinensis folium. Methods The anti-endotoxin effect of ICFWD in vitro was tested using the limulus agglutination assay. Antibacterial effect for the combination of ICFWD in vitro with cefotaxime, levofloxacin and gentamicin against 25 strains including methicillin-sensitive Staphylococcus aureus （MSSA）, methicillin-resistant Staphylococcus aureus （MRSA）, ESBLs-producing Escherichia coli non-ESBLs-producing Escherichia coli, and Pseudomonas aeruginosa （P. aeruginosa） were also investigated by the agar 2-fold dilution assay. The anti-inflammatory effect of ICFWD was observed by an xylene-induced auricle inflammation model in mice. Results ICFWD showed anti-endotoxin effects at doses ranging from 6.25 to 100mg/mL. The minimum inhibitory concentration of ICFWD against MSSA and MRSA, ESBLs-producing Escherichia coil non-ESBLs-producing Escherichia coli, as well as P aeruginosa were 8-33mg/mL, 33-〉133mg/mL and 33~133mg/mL, respectively. The combined treatment of ICFWD with cefotaxime, levofloxacin and gentamicin showed additive effects, the fractional inhibitory concentration （FIC） index were 0.5〈FIC〈 1. When orally administrated in mices, ICFWD showed anti-inflammatory effects at doses ranging from 1,280 to 2000mg/kg. Conclusion ICFWD exhibited potent anti-endotoxin effects and some anti-inflammatory effects. ICFWD had some antibacterial effects against MSSA, MRSA, ESBLs- producing Escherichia coli, non-ESBLs-producing Escherichia coli, and P aeruginosa. The combined treatment of ICFWD with cefotaxime, levofloxacin and gentamicin showed additive effects. It was indicated that the cleating-heat effect acted as the principal action in pharmacological properties of clearing-heat and detoxifying effects of ICFWD.